EP4 Human Prostanoid GPCR Binding Agonist Radioligand LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Prostanoid receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Prostanoid EP4 receptors are present in brain and many peripheral tissues (e.g., ileum>thymus>spleen>lung>heart>stomach).
Family:
GPCR
Sub Family:
Prostanoid
Class:
Class A
Protein Name:
EP4
Uniprot Number:
P35408
Protein Aliases:
PGE2 receptor EP4 subtype|Prostanoid EP4 receptor
Gene Name:
PTGER4
Gene ID:
5734
Gene Aliases:
EP4
Accession Number:
NM_000958
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]PGE2
Ligand Kd (nM):
0.3
Ligand Concentration:
0.5 nM
Non Specific:
10 µM PGE2
Incubation:
120 min at RT
Control Inhibitor:
Prostaglandin E2
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 µl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Adverse / Beneficial Action:
EP4 receptor agonism may exhibit intestinal cytoprotection, suppress hypermotility and colon cancer, reduce inflammatory activity (ulcerative colitis) and fever as well as increase wakefulness; use in the treatment of endotoxin shock and acute myocardial infarction have also been suggested. EP4 receptor antgonism may reduce intestinal mucosal and bronchopulmonary epithelial healing.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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